药剂学新剂型-201312282995.ppt

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药剂学新剂型-201312282995

Introduction of oral sustained-release and controlled-release formulations Specialty:pharmaceutics Student ID:201312282995 The basic definition of sustained-release and controlled-release formulations sustained-release formulations The preparation of the drug can for a long time sustained release drug to achieve long-lasting effect,the drug release was first-order rate process. controlled-release formulations The drug at a predetermined time automatically at a predetermined rate of release,the blood concentration for a long time constant to maintain in the effective concentration range,the drug release was zero-order or near zero-order rate process. The blood concentration-time chart of controlled-release formulations and general formulations Characteristics of sustained-release and controlled-release formulations Advantages Extended dosing interval,reduce the administration frequency,Improving medication compliance. The blood concentration is stable,avoid peak valley phenomenon,reduce the adverse effect. Lower gastrointestinal irritation. Improve the bioavailability of drugs. Reduce the total dose administered. Disadvantages Adjustment of the dose in the clinical application of lower flexibility,if a particular condition,often do not immediately stop treatment. These preparations is designed based on the mean kinetic parameters in healthy people,when the in vivo dynamics characteristic of drugs in the disease state change,can not flexibly adjust the dosing regimen. Higher production costs such these preparations,complex preparation process. Principle of sustained-release and controlled-release formulations drug delivery Dissolution mechanism. Diffusion mechanism. Corrosion and diffusion,dissolution of combining. Osmotic pressure mechanism. Ion exchange mechanism. Dissolution mechanism Noyes-whitney dissolution rate equation: By reducing the solubility of drugs,increasing the particle size of the drug,reduce the dissolution rate of the drug,allows slo

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